Invention Grant
- Patent Title: Substituted stilbenes and their reactions
- Patent Title (中): 取代的二苯乙烯及其反应
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Application No.: US13588331Application Date: 2012-08-17
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Publication No.: US08853270B2Publication Date: 2014-10-07
- Inventor: John Anthony Hadfield , Alan Thomson McGown , Stephen Patrick Mayalarp , Edward John Land , Ian Hamblett , Keira Gaukroger , Nicholas James Lawrence , Lucy Annette Hepworth , John Butler
- Applicant: John Anthony Hadfield , Alan Thomson McGown , Stephen Patrick Mayalarp , Edward John Land , Ian Hamblett , Keira Gaukroger , Nicholas James Lawrence , Lucy Annette Hepworth , John Butler
- Applicant Address: GB Salford
- Assignee: University of Salford
- Current Assignee: University of Salford
- Current Assignee Address: GB Salford
- Agency: Dann, Dorfman, Herrell and Skillman, P.C.
- Agent Patrick J. Hagan
- Priority: GB0031262.9 20001221; GB0100295.5 20010105
- Main IPC: C07C229/00
- IPC: C07C229/00 ; C07C43/18 ; A61K31/225 ; A61K31/075 ; C07C205/37 ; C07C43/23 ; C07C205/35 ; C07C46/06 ; C07C43/215 ; C07D213/68 ; C07F7/18 ; C07C50/30 ; C07C205/44 ; C07C271/22

Abstract:
The present invention relates to stilbene and quinine compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis- or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BBOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior stilbenes. These reactions include the photochemical release of an active form of the compound from a prodrug conjugate and the photochemical isomerization of the compounds, especially from a trans to cis form of compounds. The reactions can be used alone or in combination to convert inactive or comparatively less active forms of the compounds to more active forms, thereby allowing the compounds to be selectively targeted, e.g., activating them at the site of a tumor.
Public/Granted literature
- US20130023663A1 SUBSTITUTED STILBENES AND THEIR REACTIONS Public/Granted day:2013-01-24
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